UAMC00039 (dihydrochloride) |
| 时间：2023-07-15 来源：化工号 作者：C16H25Cl2N3O |
DIPEPTIDYL PEPTIDASE II抑制剂化合物UAMC 00039 DIHYDROCHLORIDE(S)-2-氨基-4-((4-氯苄基)氨基)-1-(哌啶-1-基)丁-1-酮二盐酸盐
| 中文名 | UAMC00039 (dihydrochloride)
| | 英文名 | UAMC00039 (dihydrochloride)
| | 别名 | DIPEPTIDYL PEPTIDASE II抑制剂
化合物UAMC 00039 DIHYDROCHLORIDE
(S)-2-氨基-4-((4-氯苄基)氨基)-1-(哌啶-1-基)丁-1-酮二盐酸盐
| | 英文别名 | UAMC00039
UAMC-00039
UAMC 00039
UAMC00039 2HCl
UAMC 0039 (hydrochloride)
UAMC 00039 dihydrochloride
UAMC00039 (dihydrochloride)
(2S)-2-Amino-4-[[(4-chlorophenyl)methyl]amino]-1-(1-piperidinyl)-1-butanone dihydrochloride
| | CAS | 697797-51-6
| | 化学式 | C16H25Cl2N3O
| | 分子量 | 346.3 | | 溶解度 | DMSO: ≥150 mg/mL | | 存储条件 | Inert atmosphere,Store in freezer, under -20°C | | 体外研究 | UAMC00039 has an IC 50 of 0.48±0.04 nM and a high selectivity for DPPII compared to DPPIV (IC 50 =165±9 µM) and DPP activity not caused by DPPII or DPPIV. UAMC00039 seems a promising tool to unravel the function of DPPII as well as to validate its potential as a therapeutic target. The efficacy of a DPPII inhibitor in cell culture depends not only on the inhibitors’ potency towards the enzyme but also on its stability in the medium and its ability to enter the cell. UAMC00039 is stable for at least 48 h at 37 °C in culture medium and in DPPII assay buffer. The compound is able to enter PBMC within 1 min resulting in a concentration-dependent inhibition of intracellular DPPII activity without affecting the ‘non-DPPII’ DPP activity. 1 and 100 μM UAMC00039 inhibits DPPII activity of PBMC and U937 cells more than 90%. | | 体内研究 | A dose dependent inhibition of DPPII but not of DPPIV is observed in the peripheral organs of both the rats and the mice (after oral administration) and the rabbits (after IV administration). UAMC00039 tested orally at 2 mg/kg does not cause signs of acute toxicity and does not cause any significant changes in the following functions that are evaluated: general behaviour, body temperature, respiration, bleeding time, blood pressure, urine volume, liver function, fasting glucose and gastrointestinal parameters like acidity, motility and irritation. |
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